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异狄氏剂在兔体内的代谢归宿

The metabolic fate of endrin in the rabbit.

作者信息

Bedford C T, Harrod R K, Hoadley E C, Hutson D H

出版信息

Xenobiotica. 1975 Aug;5(8):485-500. doi: 10.3109/00498257509056119.

Abstract
  1. [14C]Endrin, administered orally to rabbits, is excreted in the faeces as unchanged endrin (50% of that administered) and in the urine as a mixture of polar metabolites. 2. The major biotransformation is hydroxylation at the methylene bridge (C-12) to yield anti-12-hydroxyendrin. syn-Hydroxylation at C-12 also occurs. 3. The hydroxylated metabolites are excreted mainly as their sulphate conjugates. 4. Glucuronide conjugates are also excreted. anti-12-Hydroxyendrin is rapidly conjugated in vitro on incubation with rabbit liver microsomal glucuronyl transferase and UDPGA. 5. Comparative aspects of the metabolism of endrin in rats and rabbits are discussed.
摘要
  1. 给兔子口服[14C]异狄氏剂后,它以未变化的异狄氏剂形式(占给药量的50%)经粪便排泄,以极性代谢物混合物的形式经尿液排泄。2. 主要的生物转化是在亚甲基桥(C-12)处发生羟基化,生成反式-12-羟基异狄氏剂。C-12处也会发生顺式羟基化。3. 羟基化代谢物主要以其硫酸盐结合物的形式排泄。4. 葡糖醛酸结合物也会排泄。反式-12-羟基异狄氏剂在与兔肝微粒体葡糖醛酸基转移酶和UDPGA一起温育时,在体外会迅速结合。5. 讨论了大鼠和兔子体内异狄氏剂代谢的比较情况。

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